Background: Inhibition activity of the epigenetic readers such as bromodomain and extra-C terminal domain protein family is of high significance in many therapeutic applications due to their ability to regulate gene expression as well as the chromatin structure by binding to acetylysine residues. Objectives: In order to effectively and quickly determine the inhibition activity of these compounds for the desired therapeutic application, this work presents a grid search-based extreme learning machine computational intelligence method through which the inhibition activity of forty different compounds of substituted 4-phenylisoquinolinones was determined. Methods: The prediction and generalization capacity of the developed model were assessed using four different error metrics including root mean square error, mean absolute error, mean absolute percentage deviation and correlation coefficient between the measured values and predicted activities. The lead compound (37), together with kinase inhibitor, LY294002 and a bromodomain and extra-C terminal inhibitor, CPI-0610 were docked with a bromodomain-containing protein 4 bromodomain 1, 6P05. Results: The developed model performed better than the existing model with percentage improvement of 44.48%, 35.08%, 20.44% and 1.23% on the basis of mean absolute percentage deviation, mean absolute error, root mean square error and correlation coefficient, respectively. The lead compound has a better binding score than LY294002 and CPI-0610. Conclusion: Implementation of the developed model would be of immense guide in searching for anti-inflammatory as well as anticancer agents for effective therapeutic application.

Radon gas is by far the most important source of ionizing radiation among those that are of natural origin. In this study, radon was measured in some homes built of different types of building materials in Akoko region of Ondo state, Nigeria. The test was conducted using Accustar alpha track long term passive test devices containing CR-39 solid state nuclear track detector foil. The detectors were exposed for a period of six months. After removal the detectors were subsequently etched electrochemically and counted with computer aided image analysis system. The results show that radon concentration varies between 15.00 Bqm-3 to 141.00 Bqm-3 with a mean of 35.54 Bqm-3 and geometric mean of 29.95 Bqm-3. Annual exposure varied between 0.10 WLM to 0.17 WLM with a mean of 0.13 WLM, annual effective dose varied between 0.38 mSvy-1 to 0.69 mSvy-1 with a mean of 0.50 mSvy-1 and lifetime fatality risk varied between 0.50x10-4 to 0.85x10-4 with a mean of 0.64x10-4 in bedroom, living room, store and lobby. This study shows that the local soil origin greatly contributes to radon concentrations recorded in these areas.

No abstract

The gamma dose rate exposure levels from different brands of building materials at commercial distribution stores/shops in two major cities in Ondo State, Nigeria, were measured using a well calibrated Inspector 1000 scintillator detector. The results showed that the different brands of building materials which are Corrugated iron sheet, Aluminum roofing sheets, Conduit pipes, Paints, Cement, PVC pipes, Wash hand basin, Bath tub, Water closet, Kitchen zinc, Asbestos, Floor tiles, Wall tiles, Bullet proof door, Binding wire, rings and rods, Red bricks, Galvanized pipes, Copper pipes, Water tanks contributed excess annual effective doses of 0.332 mSv/y and 0.311mSv/y to store keepers in Ikare Akoko and Akure cities respectively. The indoor and outdoor annual effective dose of each of the investigated two cities are correlated using simple linear regression equations. The results of the modeling and experiment show that annual effective dose received by the occupants of these shops/stores was about 12 % higher than what could be received in a typical natural radiation environment in the two cities because the building materials acts as a source of radiation indoor. The research indicated that the typical habit of using poorly ventilated and confined space as stores/shops by the sales men might subject them to internal exposure through inhalation of radon gas and its short-lived decay products. Implementation of the developed equations would definitely promote rapid determination of outdoor annual effective dose through indoor annual effective dose and ultimately save time and other valuable resources.

The data obtained were used to realize the outdoor gamma radiation map of the study area.